Signal Transduction - GPCR Flashcards

1
Q

What receptor is shown?

A

GPCR

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2
Q

Can the effector of a GPCR be an ion channel?

A

Yes

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3
Q

Where does the receptor exist in a GPCR?

A

Plasma membrane

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4
Q

What 2 receptors can the G protein activate?

A

Enzyme or ion channel

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5
Q

What are seconds messengers?

A

Transfer a signal from the membrane to the rest of the cell

After (receptor activation)

soluble products

intracellular site of action

amplify the response

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6
Q

When the ligand activates the GPCR, is the signal continuous?

A

Yes

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7
Q

What is the chain of events in the GPCR?

A
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8
Q

What do second messengers do?

A
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9
Q

What are 4 examples of effectors in a GPCR?

A
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10
Q

What are examples of GPCR? (receptor)

A
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11
Q

What is the second messenger of adenylate cyclase effector?

A

cAMP

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12
Q

What is reaction of adenylate cyclase to camp?

A

ATP to CAMP + PPi

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13
Q

Can adenylate cyclase link inhibitory and stimulatory receptors?

A

Yes

regulated by Gs and Gi

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14
Q

What are the stimulating receptors adenylate cyclase?

A

Beta adrenergic

ACTH

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15
Q

What are the inhibitory receptors of adenylate cyclase?

A

Alpha 2 receptors

Muscarunic

Opiate

GABA b

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16
Q

What does camp activate?

A

PKA

17
Q

What does the inhibitory GPCR cause? (Gi, no cAMP)

A

M2, Ach R = Decreased HR

Alpha2:

Inhibitory neurotransmitter release

Contraction in smooth muscle

inhibition of insulin

18
Q

What is the effect of activating the inhibitory opioid GPCR? (no cAMP)

A

SEDATION…

19
Q

What are the sites if action of opioid analgesics?

A

Peripheral

Spinal

Supraspinal (medulla, thalamus, cortex)

20
Q

What is the best known opioid anagesic?

A

Morphine

21
Q

What is the most commonly prescribed opioid analgesic?

A

Codeine

22
Q

What are naturally occurring opioids?

A

Endorphins

23
Q

What are compounds related to opioids?

A

Methadone

Dimorphine (heroine)

Fentanyl

24
Q

What G protein activates PLC?

A

Gq

25
Q

What are the second messenger of PLC?

A

IP3
DAG

26
Q

What is the pathway of PLC (effector) in the GPCR?

A
27
Q

What can GPCR also be called?

A

metabotropic receptors

28
Q

What are the second messengers of PLC?

A

IP3

DAG

29
Q

What activates the Gi (regulates adenylate cyclases)?

A

opioid agonists

30
Q

What does increased cAMP in the cell cause? (activate PKA)

A
31
Q

What are the contradictory effects of giving someone adrenaline?

A

Beta2 receptor increases glycogen and fat metabolism in liver, fat and muscle cells

Beta1 receptor increases activity of voltage activated calcium channels in heart cells

32
Q

Opioids inhibit AC and there for decreased cAMP and PKA levels, what is the effect of this?

A

PKA does not phosphorylate K+ channel or Ca2+ channel

this open the K+ and closes the Ca2+

hyperpolarisation

inhibition of AP

33
Q

What receptor do opioid analgesics use?

A

mu receptors mainly for analgesic effects

3 types: mu, kappa, delta

34
Q

What type of effector is PLC?

A

membrane bound enzyme

35
Q

What does IP3 do? (PLC pathway)

A

increase in intracellular Ca2+

36
Q

What does DAG do? (PLC pathway)

A

activation of PKC

37
Q

IP3 increases Ca2+ in the cell, what does this result in?

A
38
Q

DAG activates PKC, what does this result in?

A